Working Paper
Authors
- Vijayagopal Gopalsamuthiram Virginia Commonwealth University ,
- Dang Ho Virginia Commonwealth University ,
- Cheryl Peck Virginia Commonwealth University ,
- Vasudevan Natarajan Virginia Commonwealth University ,
- Toolika Agrawal Virginia Commonwealth University ,
- Justina Burns Virginia Commonwealth University ,
- John Blachert Virginia Commonwealth University ,
- Daniel Cook Virginia Commonwealth University ,
- Rodger Stringham Virginia Commonwealth University ,
- Ryan Nelson Virginia Commonwealth University ,
- Saeed Ahmad Virginia Commonwealth University ,
- Frank Gupton Virginia Commonwealth University ,
- David Snead Virginia Commonwealth University ,
- Tyler McQuade Virginia Commonwealth University ,
- Rajappa Vaidyanathan Virginia Commonwealth University ,
- Kai Donsbach Virginia Commonwealth University ,
- Joshua Sieber
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Virginia Commonwealth University & Medicines for all institute
Abstract
A concise and practical synthesis has been developed to provide the 8-fluoro-5-hydroxy-3,4-diydrocarbostyril (8-FDC) fragment of OPC-167832 in 41 % yield and in > 99 % purity over 4 steps from 3-amino-4-fluorophenol. The key feature of this process is the development of a telescoped one pot synthesis of the quinolone via a chemoselective amidation and easier product isolation without the need for a column chromatography.
Content
